187 results about "Fluorouracilum" patented technology

The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising a sulfonamide compound, a sulfonate compound or a salt of them, which is represented by the following formula: (wherein ring A represents an aromatic ring which may have a substituent group; ring B represents a 6-membered unsaturated hydrocarbon ring which may have a substituent group etc.; ring C represents a 5-membered hetero-ring containing one or two nitrogen atoms, and the ring C may have a substituent group; W represents a single bond or -CH=CH-; X represents -NH- etc.; and Y represents a carbon atom or a nitrogen atom; and Z represents -NH- etc.), particularly N-(3-chloro-1H-indol-7-yl)-4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) irinotecan hydrochloride trihydrate; (2) mitomycin C; (3) 5-fluorouracil; (4) cisplatin; (5) gemcitabine hydrochloride; (6) doxorubicin; (7) taxol; (8) carboplatin; (9) oxaliplatin; (10) capecitabine; and (11) a salt of the above-mentioned (1) to (10).

The invention relates to biodegradable fluorouracil(Fu) polyester drug-bearing manoparticles with a coating material of polylactic acid, polylactic acid-glycolic acid, polylactic acid-polyethylene glycol block copolymer or polylactic acid-glycolic acid-polyethylene glycol block copolymer and the producing method including: firstly, fully dissolving the copolymer in the dichloromethane, under the ultrasonic shock, injecting the fluorouracil NaOH solution in the dichloromethane solution, dispersing uniformly, forming W / O primary latex, and beating up the primary latex and injecting into the fluorouracil saturated water solution containing 5 wt% of polyvinylalcohol (PVA), and storing in the refrigeratory after freeze-dry. The drug-bearing manoparticle has a drug content which is 10-25% of the microparticle mass, and has a smooth surface, an even diameter distribution, a remarkable slow release function and not adhesive. The micropartical size is 100-1000nm.

The invention relates to a degradable drug loading stent and a preparation method of the degradable drug loading stent. The degradable drug loading stent is characterized by comprising a skeleton structure made of a medical degradable metal or an alloy of the metal, a degradable macromolecular transition layer adhered to the surface of the skeleton structure and a drug loading layer. The degradable metal / macromolecular / drug multilayer composite stent provided by the invention has excellent mechanical property, degradable property and biocompatibility, and such drugs as taxol, taxol derivative, actinomycin D, 5-fluorouracil and sirolimus are loaded to the stent to perform active directional treatment on the focus position, so the stent is a functional degradable stent. The degradable multifunctional drug loading stent provided by the invention is suitable for interventional therapy in the blood vessel field and non-blood vessel fields and is especially suitable for interventional therapy of stenosis, obstruction or tumor of such non-blood vessel cavities as esophagus, bile duct, ductus pancreaticus, intestinal tract, urethral canal, trachea and bronchus, etc.

The present invention provides a medicinal composition having an excellent antitumor activity. That is, it provides a medicinal composition comprising a sulfonamide compound, a sulfonate compound or a salt of them, which is represented by the following formula: wherein ring A represents an aromatic ring which may have a substituent group; ring B represents a 6-membered unsaturated hydrocarbon ring which may have a substituent group etc.; ring C represents a 5-membered hetero-ring containing one or two nitrogen atoms, and the ring C may have a substituent group; W represents a single bond or -CH=CH-; X represents -NH- etc.; and Y represents a carbon atom or a nitrogen atom; and Z represents -NH- etc.), particularly N-(3-chloro-1H-indol-7-yl) -4-sulfamoylbenzenesulfonamide or a salt thereof, combined with at least one substance selected from (1) irinotecan hydrochloride trihydrate; (2) mitomycin C; (3) 5-fluorouracil; (4) cisplatin; (5) gemcitabinehydrochloride; (6) doxorubicin; (7) taxol; and (8) a salt of the above-mentioned (1) to (7).

Pharmaceutical composition comprising a chemotherapeutic agent and a TGF-beta antisense oligonucleotide, wherein the antisense oligonucleotide reduces the sensitivity and IC50, respectively, of the cytotoxicity of the chemotherapeutic agent. Preferably, the antisense oligonucleotide is a TGF-beta 1, 2, and / or 3 antisense oligonucleotide and the chemotherapeutic agent is preferably gemcitabine, 5-fluorouracil, temozolomide, dacarbacine, docetaxel, cisplatin, oxaliplatin, tamoxifen, or irinotecan.

The invention discloses a method for simultaneously detecting multiple anti-tumor drugs in a blood sample. A pretreated sample to be detected is detected by adopting ultra-high performance liquid chromatography-tandem mass spectrometry (HPLC-MS / MS). The pretreatment process comprises the following steps: adding serum into a mixed solution of methanol and acetonitrile, oscillating and centrifuging,taking out the centrifuged supernatant, drying, dissolving the dried powder into a methanol aqueous solution, and filtering to obtain a sample to be detected. The method can be used for simultaneously detecting 13 kinds of anti-tumor drugs such as methotrexate, 5-fluorouracil, apatinib, busulfan, carboplatin, cyclophosphamide, docetaxel, gemcitabine, imatinib, illinotecan, lenalidomide, oxaliplatin, paclitaxel and the like in blood.

The invention discloses a responsive chitosan microsphere / cellulose hydrogel drug-loading composite membrane and preparation thereof. The preparation includes: preparing chitosan microspheres that load tetracycline hydrochloride which is an antibacterial drug; dispersing the prepared chitosan microspheres and 5-fluorouracil evenly in three-dimensional network structure formed by crosslinking carboxymethyl cellulose and cystamine dihydrochloride, wherein 5-fluorouracil is an anticancer drug. The responsive chitosan microsphere / cellulose hydrogel drug-loading composite membrane has good biocompatibility and reduction response, can release tetracycline hydrochloride and 5-fluorouracil in controlled manner in cancer tissue areas, and has antibacterial and anticancer functions.

Oil-in-water emulsion formulations contain both free fluorouracil and fluorouracil impregnated in porous microparticles. The formulations are suitable for topical administration, and are useful for the treatment of solar keratoses, actinic keratoses, and superficial basal cell carcinomas.

The present invention provides a method for producing a cytosine deaminase (CD)-expressing, 5-fluorouracil (5-FU)-resistant microorganism which can grow in anaerobic tumor tissues, can express CD, and has a resistance to 5-FU at a concentration that is at least effective for antitumor activity. More specifically, the method is a method (A) comprising performing subculture or acclimation culture of a CD-expressing microorganism which can grow in anaerobic tumor tissues, in the presence of 5-fluorocytosine (5-FC), or a method (B) comprising (1) performing subculture or acclimation culture of a microorganism which can grow in anaerobic tumor tissues and does not express CD, in the presence of 5-FU to produce a 5-FU-resistant microorganism and (2) transforming the 5-FU-resistant microorganism by introducing a CD gene. The present invention also provides the CD-expressing, 5-FU-resistant microorganism and a pharmaceutical composition comprising the microorganism.

The invention relates to a method for loading 5-fluorouracil by using a metal-organic framework material. The method comprises the following steps: adding the nanoscale metal-organic framework material (MOF) synthesized by a hydrothermal method into a 5-fluorouracil aqueous solution; and carrying out operations such as stirring, gradient cooling, filtering, centrifugalizing, freezing and drying and the like to prepare the MOF / 5-fluorouracil compound. The drug loading method has the advantages of controlled drug release, simple operation, no organic solvents and the like.

The invention provides preparation and application of nano metal-organic framework material PCN-223 based on porphyrin ligand. The invention relates to a preparation method and application of a metal-organic framework material. The invention aims at solving the problems that an existing carrier material used for loading a medicine 5-fluorouracil is poor in drug carrying performance and drug release performance. The preparation comprises the following steps of I, the synthesis of 5,10,15,20-tetra(4-methoxycarbonylphenyl)porphyrin; II, the synthesis of [5,10,15,20-tetra(4-methoxycarbonylphenyl)porphyrin] ferric chloride; III, the synthesis of organic ligand Fe(III)-TCPPCl; IV, the synthesis of the nano metal-organic framework material PCN-223. The maximum drug carrying amount of the nano metal-organic framework material PCN-223 prepared by the invention can reach 0.344g / g. The release performance of the medicine is also higher; the release rate can reach 90 percent. The convenience is provided for loading different medicines.

The invention relates to a lactose acidized glycyrrhetinic chitosan material and a preparation method and the application thereof. The lactose acidized glycyrrhetinic chitosan material is a glycyrrhetinic acid and lactobionic acid jointly modified chitosan material which is synthesized through N-acylation reaction with chitosan serving as carrier and glycyrrhetinic acid and lactobionic acid serving as ligands. The invention further provides a lactose acidized glycyrrhetinic chitosan / 5-fluorouracil medicine carrying nano particle. The lactose acidized glycyrrhetinic chitosan material and the preparation method and the application thereof have the advantages that the dual-ligand co-modified chitosan material is synthesized for the first time, and the nano particle is prepared for target research; and the lactose acidized glycyrrhetinic chitosan which is prepared into the nano particle has higher liver targeting performance and hepatoma cell receptor mediate initiative targeting performance as compared with GA (glycyrrhetinic acid )-CTS (chitosan) and CTS, distribution in other visceral organs can be evidently reduced, reliability in hepatoma targeting is improved, and the lactose acidized glycyrrhetinic chitosan material can be used as a carrier material which has wide application prospect in clinical hepatoma targeted treatment.

The invention relates to an aromatic ruthenium complex and a synthetic method thereof. According to the technical scheme, the aromatic ruthenium complex has a structure as shown in formulas (I), (II), (III) and (IV). The method comprises the following steps of: a, placing an aromatic dichloride ruthenium dimer and a chelating diamine ligand into a methanol solution to obtain the aromatic ruthenium complex; b, placing the aromatic dichloride ruthenium dimer and a schiff bases chelating diamine ligand into the methanol solution to obtain the aromatic ruthenium complex; c, placing aromatic dichloride ruthenium dimer and 5-fluorouracil containing schiff bases chelating diamine ligand into the methanol solution to obtain the aromatic ruthenium complex; and d, reacting an aldehyde group containing anti-cancer drug or an anti-cancer drug with the aldehyde group introduced by drug modification with a chelating diamine compound to obtain the schiff bases chelating diamine ligand; and then hitching into the aromatic ruthenium complex. According to the scheme, a 5-fluorouracil aromatic ruthenium complex with anticancer synergistic effect can be prepared.

The invention provides a fluorouracil-dextran conjugate and its preparing process, which comprises, derivatizing fluorouracil, introducing acetic acid groups onto the N1 position of fluorouracil, carrying out esterification reaction by utilizing the hydroxyl on the carboxyl and the dextran, thus obtaining fluorouracil-dextran macromolecular precursor medicament.

A therapeutic approach to prevent drug resistance and chemotherapy-related secondary cancer associated with DNA mismatch repair (MMR) deficiency is disclosed based on screening antioxidants for reducing microsatellite instability (MSI) while enhancing the cytotoxicity of chemotherapeutic agents. The work is based on experiments using antioxidants to target reactive oxygen species generated by oxaliplatin, a commonly used chemotherapeutic agent, and is applicable to other chemotherapeutic agent, and in particular 5-fluorouracil, methotrexate, CCNU, etoposide and vinblastine. In particular oxaliplatin is co-treated with an antioxidant, including CDC, CAPE, ciclopirox ethanolamine, hinokitiol, gossypol, n-Octyl caffeate, baicalein, or curcumin.

The invention relates to a method for preparing tegafur, which belongs to the field of drug synthesis. Follow the steps below: (1) Weigh 2,3-dihydrofuran and ethanol into the flask, add solvent tetrahydrofuran to it, then weigh 5-20% of the total mass of raw materials CuCl2, microwave irradiation 250W, react at 25°C for 0.6h. (2) Cool to room temperature, then add 5-fluorouracil with a molar ratio of 3:10 to 2,3-dihydrofuran, microwave irradiation 200-600W, reaction temperature 60-130°C, and react for 0.7h; After boiling the solvent, an oily substance was obtained; washed with ether to obtain a white solid, and the obtained solid was recrystallized with absolute ethanol to obtain the product. The process does not use toxic solvent chloroform, does not use high-boiling point solvents, and the one-step production cost is low. Microwave irradiation-assisted synthesis can speed up the reaction rate, and is widely used in organic substitution reactions.

The invention discloses a method for determining the concentrations of two anti-tumor drugs, metabolites and endogenous substances related to the activity of a metabolic enzyme in human plasma, whichcomprises the following steps: preprocessing, respectively taking voriconazole and bromouracil as internal standards, separating drug components in supernate by using high performance liquid chromatography in a preprocessed sample, performing drug targeting detection by using a high-resolution mass spectrum multi-reaction monitoring mode, and quantifying to realize the analysis and determination of the concentrations of the two anti-tumor drugs, the metabolites and the endogenous substances related to the activity of the metabolic enzyme in the plasma. The method has the advantages of rapidness, extremely high targeting property, high flux, high sensitivity, strong specificity, good precision and accuracy, good stability, high extraction recovery rate, no obvious matrix effect and dilutioneffect and the like. The method for determining the concentrations of two anti-tumor drugs, metabolites and endogenous substances related to the activity of the metabolic enzyme in the human plasma can be used for monitoring the blood concentration of irinotecan and metabolites thereof and the blood concentration of fluorouracil and endogenous substances related to the activity of the metabolic enzyme thereof clinically.

The invention discloses a PEG (polyethylene glycol) modified recombinant arginine deiminase (ADI) as well as a preparation method and application thereof, belonging to the technical field of biomedical engineering. The stability of ADI-PEG obtained by modifying ADI with PEG in vitro and in mouse plasma is remarkably improved. A pharmacokinetics / pharmacodynamics study shows that compared with free ADI before modification, the half-life period of ADI-PEG in a mouse is prolonged by more than 11 times; the concentration of arginine in the plasma can be reduced and maintained for more than 5 days in the limiting level through single injection of 5U ADI-PEG and can be maintained for 1 day only through injection of unmodified ADI; an H22 liver cancer model mouse is treated for 15 days, and the cancer cell inhibition rate of ADI-PEG (15U) is 95.02% close to 98.34% (the inhibition rate) of a positive control group treated with 5-fluorouracil. PEG modified recombinant arginine deiminase is relatively long in in-vivo half-life period and relatively low in immunogenicity, and serves as an excellent tumor treating or inhibiting drug.

The invention belongs to the field of organic chemistry synthesis and particularly relates to a method for preparing 5-fluorouracil. The method comprises the following steps: (1) after nitrogen displacement, adding sodium methoxide into toluene, then dripping part of ethyl formate at first, then dripping methyl fluoroacetate and the rest ethyl formate, and stirring after dripping for reaction; (2) adding methyl alcohol and sodium methoxide, stirring, reducing the temperature to 15-25 DEG C, adding urea for reaction, removing a solvent after reaction, re-adding water, cooling, stirring, regulating the pH to 3-4, and filtering to obtain the product. According to the invention, as ethyl formate and methyl fluoroacetate are mixed and dripped, and the dripping temperature is reduced, loss of ethyl formate is reduced, accordingly, reaction of ethyl formate and methyl fluoroacetate is promoted, and the yield is improved to be more than 74.5%; addition of the solvent is reduced, so that the solvent reclamation amount can be remarkably reduced and the manufacturing cost is greatly lowered.

The invention discloses a pharmaceutical co-crystal of 5-fluorouracil and L-phenylalanine and a preparation method of the pharmaceutical co-crystal, and relates to the field of pharmaceutical co-crystals. The 5-fluorouracil-phenylalanine co-crystal is [C4H3FN2O2*C9H11NO2], and a basic structural unit is formed from a 5-fluorouracil molecule and an L-phenylalanine molecule. The co-crystal belongs to the orthorhombic system, and the space group is P212121. 5-fluorouracil and L-phenylalanine are used as raw materials, and the pharmaceutical co-crystal is prepared by adopting solvent evaporation method and cooling method. According to the pharmaceutical co-crystal disclosed by the invention, the solubility of 5-fluorouracil is improved, and a foundation is laid for improving the bioavailability and the drug effect of 5-fluorouracil. The preparation method of the pharmaceutical co-crystal is simple and easy to implement, low in cost and convenient to popularize in industrial pharmacy on a large scale.

The invention discloses a 5-fluorouracil-caffeic acid eutectic crystal and a preparation method of the co-crystal, and relates to the field of pharmaceutical co-crystals. The composition of the 5-fluorouracil-caffeic acid eutectic crystal is [C4H3N2O2F.C9H8O4.2H2O], and a basic structural unit is formed by a 5-fluorouracil molecule, a caffeic acid molecule and two water molecules. The pharmaceutical 5-fluorouracil-caffeic acid eutectic crystal belongs to a triclinic system, and the space group is P-1. 5-fluorouracil and caffeic acid are used as raw materials, and the eutectic crystal is prepared by adopting a solvent evaporation method and a cooling method. According to the pharmaceutical 5-fluorouracil-caffeic acid eutectic crystal, the solubility of the 5-fluorouracil is improved, and afoundation is laid for improving the bioavailability and the drug effect of the 5-fluorouracil. The preparation method of the pharmaceutical 5-fluorouracil-caffeic acid eutectic crystal is simple andeasy to implement, low in cost and convenient to popularize in industrial pharmacy on a large scale.

The present invention relates to intraocular lenses. At present, the polymethyl methacrylate (PMMA) intraocular lens commonly used in clinic for the treatment of cataract often causes inflammation after being implanted in the human body. Posterior capsule turbidity is also the main complication after cataract surgery. To solve these problems, the present invention selects antineoplastic drugs According to the weak penetrability of chitosan nanoparticles in the eye and the characteristics that the phagocytosis of conjunctival epithelial cells on nanoparticles is related to the size of the nanoparticles, chitosan-polyacrylic acid was used as a carrier to prepare fluorouracil nanoparticles Formulation, mixed coating on the surface of PMMA intraocular lens. The present invention also provides the preparation method of the above-mentioned intraocular lens. The invention not only increases the biocompatibility of the intraocular lens, inhibits the opacity of the posterior capsule after the implantation of the intraocular lens, but also prevents the anterior membrane and post-cataract after the implantation of the intraocular lens.

The invention discloses an application of vanillin in preparation of a nicotinamide-N-methyltransferase inhibitor. The inhibitor is prepared from traditional Chinese medicine monomer vanillin and pharmaceutically acceptable auxiliary materials. According to the invention, proliferation of various colorectal cancer cell strains is inhibited by inhibiting the expression of NNMT and enzyme activity in vitro and vivo, and an anti-tumor effect is achieved. Studies show that vanillin can weaken the drug resistance of colorectal cancer cell strains to 5-FU caused by high expression of NNMT in vitro,so that the chemotherapy sensitivity is enhanced; the apoptosis of the colorectal cancer cell strains with high expression of NNMT is increased by inducing ROS production and mitochondrial damage in cells; and the inhibitory effect of 5-fluorouracil on tumor proliferation and the apoptosis rate can be improved, so as to enhance the chemotherapy effect. The vanillin can be used as an NNMT inhibitorfor preparing anti-colorectal cancer drugs or adjuvant chemotherapy drugs, and has a good application prospect.

The invention relates to an application of salvianolic acid L in preparation of medicines used for treating tumor, salvianolic acid L belongs to a phenolic acid compound which is a novel water-soluble compound with a confirmed structure extracted from a traditional Chinese medicine red sage root, a pharmacological research shows that the phenolic acid possesses anti-oxidation effect and anti-myocardial ischemia effect. According to the invention, the salvianolic acid L induces the apoptosis of tumor cells and also can kill the tumor cells. Animal experiments show that salvianolic acid L possesses certain antineoplastic activity and does not appear toxicity, and is capable of substantially enhancing antineoplastic activity of various tumor medicines 5-fluorouracil, mitomycin C and the like, the compound is expected to be used for clinical tumor treatment.

The present invention relates to a new dosage form of antineoplastic fluorouracil-nano particle preparation and its preparation method. Said invention adopts chitosan-polyacrylic acid nano particles as carrier, so that it has good biological compatibility and adhesion property, the grain size of the nano particle is 50-250 nm. Said fluorourocil can be made into nano particle dry powder preparation.

The invention discloses a silk fibroin-based nanodrug for targeted combined chemotherapy of breast cancer, and a preparation method thereof. The nanodrug loaded with curcumin (CUR) and 5-fluorouracil(5-FU) is prepared through a solvent volatilization process by using regenerated silk fibroin as a carrier, and the surface of the nanodrug is modified with a targeted molecule hyaluronic acid (HA). The above nanoparticle has a small hydrated particle size (198.0 + / - 1.8 nm), a good size uniformity (PDI: 0.097), a high drug loading capacity (CUR: 2.1%; 5-FU: 1.7%) and a good dispersibility, is notprone to agglomerate, and is convenient to construct multifunctional drug-loaded silk fibroin nanoparticles. The silk fibroin-based targeted nanodrug obtained in the invention can effectively inhibittumor cell proliferation and increase the concentration of the anticancer drug in the cells. The hyaluronic acid (HA) for modifying the surface enhances the therapeutic effect of single drugs on thebreast cancer and achieves synergistic effects in cancer treatment.

Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS-, HO- or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5'-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=-NH2, -OH, -COOH, -O-CO-R-COR*, -NH-CO-R-COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R*H, phenyl, alkyl with 1-6 carbon atoms.

The invention discloses series of compounds of fluorouracil in 1- or 3-triazole rings and a preparation method of compounds, belongs to the field of medicinal chemistry, and particularly relates to a novel fluorouracil antitumor compound with the following general formula of chemical structure. The fluorouracil compound has antitumor activity; and the preparation method is economical, simple, mild and efficient.

The invention provides a 5-fluorouracil copolymer with anti-tumor activity. 5-fluorouracil or 5-fluorouracil and sulfadiazine is or are connected to N-(2-hydroxypropyl) methacrylamide through a polymerization mode to form a macromolecule copolymer with good biological compatibility. The macromolecule copolymer is used for connecting the 5-fluorouracil with anti-tumor activity and the sulfadiazine to a tumor targeted drug carrier N-(2-hydroxypropyl) methacrylamide to ensure that the anti-tumor activity is overlapped, further the inhibition of the macromolecule polymer to tumors is promoted, and the standing time of anti-tumor drugs in tumors is greatly prolonged; and meanwhile, by adopting the macromolecule carrier HPMA (hydroxypropyl methacrylate), the toxicity of the anti-cancer drugs is reduced, the hurt to normal tissues is decreased, and a new idea is provided for preparing novel anti-tumor drugs.